Subclassification of atrial and intestinal muscarinic receptors of the rat--direct binding studies with agonists and antagonists.

abstract：:1. The purpose of the present study was to identify and investigate the role of 5-hydroxytryptamine3 (5-HT3) receptors in the area postrema in the control of cisplatin-induced emesis in the ferret. 2. Homogenate binding and autoradiography experiments using the high affinity 5-HT3 receptor ligand, [3H]-GR65630, identi...

journal_title：British journal of pharmacology

authors： Higgins GA,Kilpatrick GJ,Bunce KT,Jones BJ,Tyers MB

更新日期：1989-05-01 00:00:00

abstract：:The intravenous administration of naloxone 2 min before coronary artery occlusion in anaesthetized dogs reduced the incidence and severity of cardiac arrhythmias during coronary occlusion (20 min) and reperfusion (120 min) in a dose-related manner. It also reduced the mortality. At a dose of 1 mg kg-1 (the maximum dos...

journal_title：British journal of pharmacology

authors： Huang XD,Lee AY,Wong TM,Zhan CY,Zhao YY

更新日期：1986-03-01 00:00:00

abstract：BACKGROUND AND PURPOSE:alpha5IA (3-(5-methylisoxazol-3-yl)-6-[(1-methyl-1,2,3-triazol-4-yl)methyloxy]-1,2,4-triazolo[3,4-a]phthalazine) is a triazolophthalazine with subnanomolar affinity for alpha1-, alpha2-, alpha3- and alpha5-containing GABA(A) receptors. Here we have evaluated the relationship between plasma alpha5...

journal_title：British journal of pharmacology

authors： Atack JR,Eng WS,Gibson RE,Ryan C,Francis B,Sohal B,Dawson GR,Hargreaves RJ,Burns HD

更新日期：2009-07-01 00:00:00

abstract：:An approximate eight fold desensitization of the circular coat of the distal rabbit colon to adenosine 5'-triphosphate (ATP) and adenosine could be achieved by repeatedly exposing the organ to relatively low concentrations (10-100 microM) of these compounds. The desensitization was specific and reversible after prolon...

journal_title：British journal of pharmacology

authors： Crema A,D'Angelo L,Frigo GM,Lecchini S,Onori L,Tonini M

更新日期：1982-02-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Quercetin is a natural polyphenolic flavonoid that displays anti-diabetic properties in vivo. Its mechanism of action on insulin-secreting beta cells is poorly documented. In this work, we have analysed the effects of quercetin both on insulin secretion and on the intracellular calcium concentrat...

journal_title：British journal of pharmacology

authors： Bardy G,Virsolvy A,Quignard JF,Ravier MA,Bertrand G,Dalle S,Cros G,Magous R,Richard S,Oiry C

更新日期：2013-07-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Inhaled glucocorticoid (ICS)/long-acting β2 -adrenoceptor agonist (LABA) combination therapy is a recommended treatment option for patients with moderate/severe asthma in whom adequate control cannot be achieved by an ICS alone. Previously, we discovered that LABAs can augment dexamethasone-induc...

journal_title：British journal of pharmacology

authors： Joshi T,Johnson M,Newton R,Giembycz MA

更新日期：2015-05-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Pyrazole derivatives have recently been suggested as selective blockers of transient receptor potential cation (TRPC) channels but their ability to distinguish between the TRPC and Orai pore complexes is ill-defined. This study was designed to characterize a series of pyrazole derivatives in term...

journal_title：British journal of pharmacology

authors： Schleifer H,Doleschal B,Lichtenegger M,Oppenrieder R,Derler I,Frischauf I,Glasnov TN,Kappe CO,Romanin C,Groschner K

更新日期：2012-12-01 00:00:00

abstract：:1. Microvascular permeability in the mesentery and consequent leakage of protein into the peritoneum of spontaneously hypertensive rats (SHR) and normotensive rats (NTR) was measured in vivo by the extravasation of Evans blue dye. 2. In sensitized NTR, challenge with antigen produced extensive increases in dye extrava...

journal_title：British journal of pharmacology

authors： Kwasniewski FH,Tavares de Lima W,Bakhle YS,Jancar S

更新日期：1998-06-01 00:00:00

abstract：:1. Membrane effects of cromakalim (Crom; 50-300 microM) were examined in CA1 neurones recorded mainly by intracellular, single-electrode voltage-clamping in slices (from Sprague-Dawley rats) kept in an interface chamber at 33 degrees C. 2. In 14 cells held at -63 +/- 3.5 mV, in the presence of tetrodotoxin, kynurenic ...

journal_title：British journal of pharmacology

authors： Erdemli G,Krnjević K

更新日期：1994-10-01 00:00:00

abstract：:The pharmacological activity of two natural bombesin-like peptides, alytesin and litorin, and 25 related synthetic peptides has been compared to that of bombesin. 2 The minimum length of the amino acid chain required for the first appearance of bombesin-like effects was represented by the C-terminal heptapeptide, and ...

journal_title：British journal of pharmacology

authors： Broccardo M,Falconieri Erspamer G,Melchiorri P,Negri L,de Castiglione R

更新日期：1975-10-01 00:00:00

abstract：:1. The influence of sodium and potassium on the accumulation of 5-hydroxytryptamine (5-HT) by rat blood platelets was investigated.2. An absolute dependence of 5-HT uptake on the sodium concentration in the medium was found.3. Removal of potassium reduced the uptake by about 60%. High concentrations of potassium inhib...

journal_title：British journal of pharmacology

authors： Sneddon JM

更新日期：1969-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:The sarcoplasmic reticulum Ca²⁺-ATPase (SERCA) plays a role in thermogenesis. The exogenous compound capsaicin increased SERCA-mediated ATP hydrolysis not coupled to Ca²⁺ transport. Here, we have sought to identify endogenous compounds that may function as SERCA uncoupling agents. EXPERIMENTAL A...

journal_title：British journal of pharmacology

authors： Mahmmoud YA,Gaster M

更新日期：2012-08-01 00:00:00

abstract：BACKGROUND AND PURPOSE:We previously demonstrated that chronic hyperinsulinaemia induced by drinking high levels of fructose augments adrenergic nerve-mediated vasoconstriction and suppresses vasodilatation mediated by calcitonin gene-related peptide (CGRP)-containing (CGRPergic) vasodilator nerves. In this study, the ...

journal_title：British journal of pharmacology

authors： Takatori S,Zamami Y,Yabumae N,Hanafusa N,Mio M,Egawa T,Kawasaki H

更新日期：2008-04-01 00:00:00

abstract：:The modulatory effects of protein kinase C (PKC) on the activation of cytosolic phospholipase A2 (cPLA2) and adenylyl cyclase (AC) have recently been described. Since the signalling cascades associated with these events play critical roles in various functions of macrophages, we set out to investigate the crosstalk be...

journal_title：British journal of pharmacology

authors： Lin WW,Chen BC

更新日期：1998-12-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Human lung fibroblasts (HLF) express high levels of the LPA1 receptor, a GPCR that responds to the endogenous lipid mediator, lysophosphatidic acid (LPA). Several molecular species or analogues of LPA exist and have been detected in biological fluids such as serum and plasma. The most widely expr...

journal_title：British journal of pharmacology

authors： Sattikar A,Dowling MR,Rosethorne EM

更新日期：2017-02-01 00:00:00

abstract：:1. The inhibitory effect of erythrocyte suspensions and haemoglobin solutions on the response of the bovine retractor penis muscle (BRP) and the rat anococcygeus to field stimulation of their non-adrenergic non-cholinergic (NANC) nerves has been compared. Haemoglobin 3 microM greatly reduced the relaxant response in b...

journal_title：British journal of pharmacology

authors： Gillespie JS,Sheng H

更新日期：1989-10-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Recent studies suggest that the effects of cyclooxygenase-2 (COX-2) inhibition are mediated by cannabinoid receptor activation. However, some non-steroidal anti-inflammatory drugs inhibit the enzyme fatty acid amide hydrolase, which regulates levels of some endocannabinoids. Whether COX-2 directl...

journal_title：British journal of pharmacology

authors： Staniaszek LE,Norris LM,Kendall DA,Barrett DA,Chapman V

更新日期：2010-06-01 00:00:00

abstract：:In the present study we tested the effects of the antihyperalgesic compound gabapentin on dorsal horn neurones in adult spinal cord. Slices were taken from control and hyperalgesic animals suffering from streptozocin-induced diabetic neuropathy. At concentrations up to 100 microM, bath application failed to affect the...

journal_title：British journal of pharmacology

authors： Patel MK,Gonzalez MI,Bramwell S,Pinnock RD,Lee K

更新日期：2000-08-01 00:00:00

abstract：:1. Many apparent actions of adenosine 5'-triphosphate (ATP) are mediated by adenosine produced by enzymatic hydrolysis of the nucleotide. Previously described actions of ATP in the CNS have been partly due to this phenomenon. In the present study analogues of ATP, which are not hydrolysed to adenosine, were used to se...

journal_title：British journal of pharmacology

authors： Stone TW,Cusack NJ

更新日期：1989-06-01 00:00:00

abstract：:1. We have studied the mechanical response of circular strips of the guinea-pig ileum to tachykinins and characterized the receptors involved by means of receptor-selective agonists. 2. The strips responded to both substance P (SP) and neurokinin A (NKA), as well as to [Pro9]-SP sulphone (selective NK1-receptor agonis...

journal_title：British journal of pharmacology

authors： Maggi CA,Patacchini R,Giachetti A,Meli A

更新日期：1990-12-01 00:00:00

abstract：:1. Our study was aimed at investigating the duration of the bronchodilator action of the antimuscarinc drug glycopyrrolate compared to tiotropium and ipratropium. In the guinea-pig isolated trachea, the time (t1/2) necessary for a contractile response to carbachol (0.3 microM) to return to 50% recovery after washout o...

journal_title：British journal of pharmacology

authors： Villetti G,Bergamaschi M,Bassani F,Bolzoni PT,Harrison S,Gigli PM,Janni A,Geppetti P,Civelli M,Patacchini R

更新日期：2006-06-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Positive allosteric modulation of α4β2 nicotinic acetylcholine (nACh) receptors could add a new dimension to the pharmacology and therapeutic approach to these receptors. The novel modulator NS9283 was therefore tested extensively. EXPERIMENTAL APPROACH:Effects of NS9283 were evaluated in vitro ...

journal_title：British journal of pharmacology

authors： Timmermann DB,Sandager-Nielsen K,Dyhring T,Smith M,Jacobsen AM,Nielsen EØ,Grunnet M,Christensen JK,Peters D,Kohlhaas K,Olsen GM,Ahring PK

更新日期：2012-09-01 00:00:00

abstract：BACKGROUND AND PURPOSE:There is growing evidence that inflammation plays a major role in the pathogenesis of neural damage caused by deposition of amyloid β (Aβ) in the brain. Nimodipine has received attention as a drug that might improve learning and reduce cognitive deficits in Alzheimer's disease, but the mechanism ...

journal_title：British journal of pharmacology

authors： Sanz JM,Chiozzi P,Colaianna M,Zotti M,Ferrari D,Trabace L,Zuliani G,Di Virgilio F

更新日期：2012-12-01 00:00:00

abstract：:BACKGROUND AND PURPOSE The Ca(2+) paradox is an important phenomenon associated with Ca(2+) overload-mediated cellular injury in myocardium. The present study was undertaken to elucidate molecular and cellular mechanisms for the development of the Ca(2+) paradox. EXPERIMENTAL APPROACH Fluorescence imaging was performe...

journal_title：British journal of pharmacology

authors： Kojima A,Kitagawa H,Omatsu-Kanbe M,Matsuura H,Nosaka S

更新日期：2010-12-01 00:00:00

abstract：:1. The 5-hydroxytryptamine (5-HT)1A receptor agonist, 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT), has been shown to label 5-HT reuptake sites. 2. To study the functional consequences of this property, the effects of 8-OH-DPAT were compared with those of the 5-HT reuptake inhibitors, paroxetine and clomipramine...

journal_title：British journal of pharmacology

authors： Assié MB,Koek W

更新日期：1996-11-01 00:00:00

abstract：:The vanilloid receptor (VR1) is a ligand-gated ion channel, which plays an important role in nociceptive processing. Therefore, a pharmacological characterization of the recently cloned rat VR1 (rVR1) was undertaken. HEK293 cells stable expressing rVR1 (rVR1-HEK293) were loaded with Fluo-3AM and then incubated at 25 d...

journal_title：British journal of pharmacology

authors： Jerman JC,Brough SJ,Prinjha R,Harries MH,Davis JB,Smart D

更新日期：2000-06-01 00:00:00

abstract：:1. When the isolated small intestine of the rat is perfused via the mesenteric artery, an oxytocic principle (Gaddum's substance R) is released which is detectable in the perfusate after 30 min and is present in samples collected 8 h later. 2. The oxytocic activity of substance R is lost after boiling but is unaffecte...

journal_title：British journal of pharmacology

authors： Douglas GJ,Williams KI,Flower RJ

更新日期：1991-04-01 00:00:00

abstract：:1. Nine non-steroidal anti-inflammatory drugs were tested for antagonism of bradykinin-induced bronchoconstriction in guinea-pig lungs in vivo. Only one, benzydamine, was inactive.2. The descending order of potency of the active anti-inflammatory drugs was meclofenamate = Scha 306>Scha 87/2>indoxole>Mi85>indomethacin>...

journal_title：British journal of pharmacology

authors： Collier HO,James GW,Piper PJ

更新日期：1968-09-01 00:00:00

abstract：:1. Previous work from our laboratory has shown that cannabis induces aggressive behaviour in rats that have been deprived of rapid eye movement (REM) sleep. It was suggested that this effect was related to brain catecholamines, with dopamine playing an agonist role and noradrenaline an inhibitory one. The present pape...

journal_title：British journal of pharmacology

authors： Carlini EA,Lindsey CJ,Tufik S

更新日期：1977-11-01 00:00:00

abstract：BACKGROUND AND PURPOSE:Using an innovative chemical approach, peptide welding technology (PWT), a tetrabranched derivative of nociceptin/orphanin FQ (N/OFQ) has been generated and pharmacologically characterized. Both in vitro and in vivo PWT2-N/OFQ displayed the same pharmacological profile to the natural ligand. It w...

journal_title：British journal of pharmacology

authors： Rizzi A,Sukhtankar DD,Ding H,Hayashida K,Ruzza C,Guerrini R,Calò G,Ko MC

更新日期：2015-07-01 00:00:00